Kashyap Priyanka, Verma Sangeeta, Gupta Pankaj, Narang Rakesh, Lal Sukhbir, Devgun Manish
Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra, 136119 India.
Med Chem Res. 2023 May 29:1-31. doi: 10.1007/s00044-023-03077-z.
Antimicrobial resistance (AMR) is a worldwide concern among infectious diseases due to increased mortality, morbidity and treatment cost. According to WHO 2019 report, among the 32 antibiotics in the clinical trials, only six were classified as innovative and containing novel moiety. The remaining antibiotics from this list contain previously known moiety (WHO AMR 2019). Therefore, the development of novel antibiotics to control resistance problems is crucial. Benzothiazole derivatives are of great interest due to their wide range of biological activities and medicinal applications. Reported data indicated that benzothiazole derivatives displayed antibacterial activity by inhibiting the dihydroorotase, DNA gyrase, uridine diphosphate-n-acetyl enol pyruvyl glucosamine reductase (MurB), peptide deformylase, aldose reductase, casdihydrofolate reductase, enoyl acyl carrier protein reductase, dialkylglycine decarboxylase, dehydrosqualene synthase, dihydropteroate synthase and tyrosine kinase. The present review analyzed the synthesis, structure-activity relationship (SAR) and mechanism of action studies of benzothiazole derivatives as antibacterial agents reported by various research groups in the last five years (2018-2022). Different patents on the antimicrobial activity of benzothiazole derivatives have also been summarized. The finding of the present review will be beneficial for the researchers in the development of novel antibacterial molecules based on benzothiazole moiety.
由于死亡率、发病率和治疗成本的增加,抗菌药物耐药性(AMR)已成为全球传染病领域关注的问题。根据世界卫生组织2019年的报告,在临床试验中的32种抗生素中,只有6种被归类为创新型且含有新的部分。该清单中的其余抗生素含有已知的部分(世界卫生组织抗菌药物耐药性报告,2019年)。因此,开发新型抗生素以控制耐药性问题至关重要。苯并噻唑衍生物因其广泛的生物活性和药用价值而备受关注。报道的数据表明,苯并噻唑衍生物通过抑制二氢乳清酸酶、DNA回旋酶、尿苷二磷酸-N-乙酰胞壁酸还原酶(MurB)、肽脱甲酰基酶、醛糖还原酶、二氢叶酸还原酶、烯酰基载体蛋白还原酶、二烷基甘氨酸脱羧酶、脱水鲨烯合酶、二氢蝶酸合酶和酪氨酸激酶来发挥抗菌活性。本综述分析了过去五年(2018-2022年)各研究小组报道的苯并噻唑衍生物作为抗菌剂的合成、构效关系(SAR)和作用机制研究。还总结了关于苯并噻唑衍生物抗菌活性的不同专利。本综述的研究结果将有助于研究人员开发基于苯并噻唑部分的新型抗菌分子。